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化學化合物
专利权人:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED
发明人:
AXTEN, JEFFREY MICHAEL,阿克斯坦 杰佛瑞,阿克斯坦 傑佛瑞,FAUCHER, NICOLAS ERIC,佛雪 尼可拉斯,DAUGAN, ALAIN CLAUDE-MARIE,道甘 艾伦,道甘 艾倫,KETHIRI, RAGHAVA REDDY,凯西里 雷格哈瓦,凱西里 雷格哈瓦,KRISTAM, RAJENDRA,科斯谭 拉詹德拉,科斯譚 拉詹德拉,VENKA,阿克斯坦 杰佛瑞,阿克斯坦 傑佛瑞,佛雪 尼可拉斯,道甘 艾伦,道甘 艾倫,凯西里 雷格哈瓦,凱西里 雷格哈瓦,科斯谭 拉詹德拉,科斯譚 拉詹德拉
申请号:
TW105129694
公开号:
TW201722957A
申请日:
2016.09.13
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The invention is directed to substituted pyrrolidinone and imidazolidinone derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein.The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases/injuries associated with activated unfolded protein response pathways, such as Alzheimer’s disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson’s disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt-Jakob Disease, fatal familial insomnia, Gerstmann-Sträussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick’s disease, Neimann-Pick’s disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.本發明係關於經取代之吡咯啶酮及咪唑啶酮衍生物。具體地說,本發明係關於根據式(I)之化合物:其中R1、R2、R3、R4、R5、R6、R7、X及Y是根據文中的定義。本發明之化合物是PERK之抑制劑且可以用於治療癌症、癌症前徵候群及與活化未折疊的蛋白質反應通道相關的疾病,例如阿茲海默氏症、脊髓損傷、外傷性腦損傷、缺血性中風、中風、巴金森氏症、糖尿病、代謝徵候群、代謝性疾病、漢丁頓氏舞蹈症、克雅氏病(Creutzfeldt-Jakob Disease)、致死性家族性失眠、杰茨
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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